Publication Cover
Xenobiotica
the fate of foreign compounds in biological systems
Volume 33, 2003 - Issue 2
109
Views
15
CrossRef citations to date
0
Altmetric
Research Article

Many P-glycoprotein substrates do not inhibit the transport process across cell membranes

, &
Pages 131-140 | Published online: 22 Sep 2008

References

  • AMBUDKAR, S. V., CARDARELLI, C. O., PASHINSKY, I. and STEIN, W. D., 1997, Relation between the turnover number for vinblastine transport and for vinblastine-stimulated ATP hydrolysis by human P-glycoprotein. Journal of Biological Chemistry, 272, 21160–21166.
  • AMBUDKAR, S. V., DEY, S., HRYCYNA, C. A., RAMACHANDRA, M., PASTAN, I. and GOTTESMAN, M. M., 1999, Biochemical, cellular, and pharmacological aspects of the multidrug transporter. Annual Reviews in Pharmacology and Toxicology, 39, 361–398.
  • BARNES, K. M., DICKSTEIN, B., CUTLER, G. B., JR, Foy), T. and BATES, S. E., 1996, Steroid treatment, accumulation, and antagonism of P-glycoprotein in multidrug-resistant cells. Biochemistry, 35, 4820–4827.
  • BORGNIA, M. J., EYTAN, G. D. and ASSARAF, Y. G., 1996, Competition of hydrophobic peptides, cytotoxic drugs, and chemosensitizers on a common P-glycoprotein pharmacophore as revealed by its ATPase activity. Journal of Biological Chemistry, 271, 3163–3171.
  • BORREL, M. N., FIALLO, M., VERESS I. and GARNIER-SUILLEROT, A., 1995, The effect of crown ethers, tetraalkylammonium salts, and polyoxyethylene amphiphiles on pirarubicin incorporation in K562 resistant cells. Biochemical Pharmacology, 50, 2069–2076.
  • CARULLI, G., PETRINI, M., MARINI, A., VAGLINI, F., CARACCIOLO, F. and GRASSI, B., 1990, P-glycoprotein and drug resistance in acute leukemias and in the blastic crisis of chronic myeloid leukemia. Haematologica, 75, 516–521.
  • CHIBA, P., ECKER, G., SCHMID, D., DRACH, J., TELL, B., GOLDENBERG, S. and GEKELER, V., 1996, Structural requirements for activity of propafenone-type modulators in P-glycoprotein-mediated multidrug resistance. Molecular Pharmacology, 49, 1122–1130.
  • COLLETT, A., HIGGS, N. B., Sims, E., ROWLAND, M. and WARHURST, G., 1999, Modulation of the permeability of H2 receptor antagonists cimetidine and ranitidine by P-glycoprotein in rat intestine and the human colonic cell line Caco-2. Journal of Pharmacology and Experimental Therapeutics, 288, 171–178.
  • DOPPENSCHMITT, S., SPAHN-LANGGUTH, H., REGARDH, C. G. and LANGGUTH, P., 1999, Role of P-glycoprotein-mediated secretion in absorptive drug permeability: An approach using passive membrane permeability and affinity to P-glycoprotein. Journal of Pharmaceutical Science, 88,1067–1072.
  • EYTAN, G. D., REGEV, R. and ASSARAF, Y. G., 1996a, Functional reconstitution of P-glycoprotein reveals an apparent near stoichiometric drug transport to ATP hydrolysis. Journal of Biological Chemistry, 271, 3172–3178.
  • EYTAN, G. D., REGEV, R., OREN, G. and ASSARAF, Y. G., 1996b, The role of passive transbilayer drug movement in multidrug resistance and its modulation. Journal of Biological Chemistry, 271,12897–12902.
  • EYTAN, G. D., REGEV, R., OREN, G., HURWITZ, C. D. and ASSARAF, Y. G., 1997, Efficiency of P-glycoprotein-mediated exclusion of rhodamine dyes from multidrug-resistant cells is determined by their passive transmembrane movement rate. European Journal of Biochemistry, 248, 104–112.
  • FERTE, J., 2000, Analysis of the tangled relationships between P-glycoprotein-mediated multidrug resistance and the lipid phase of the cell membrane. European Journal of Biochemistry, 267, 277–294.
  • FERTE, J., KUHNEL, J. M., CHAPUIS, G., ROLLAND, Y., LEWIN, G. and SCHWALLER, M. A., 1999, Flavonoid-related modulators of multidrug resistance: synthesis, pharmacological activity, and structure-activity relationships. Journal of Medical Chemistry, 42, 478–489.
  • FISHER, G. A., Lum, B. L., HAUSDPR, J. and Sixic, B. I. 1996, Pharmacological considerations in the modulation of multidrug resistance. European Journal of Cancer, 32A, 1082–1088.
  • GOTTESMAN, M. M. and PASTAN, I., 1993, Biochemistry of multidrug resistance mediated by the multidrug transporter. Annual Reviews of Biochemistry, 62, 385–427.
  • GOTTESMAN, M. M., PASTAN, I. and AMBUDKAR, S. V., 1996, P-glycoprotein and multidrug resistance. Current Opinions in Genetic Development, 6,610–617.
  • ITo, K., KUSUHARA, H. and SUGIYAMA, Y., 1999, Effects of intestinal CYP3A4 and P-glycoprotein on oral drug absorption - theoretical approach. Pharmaceutical Research, 16, 225–231.
  • LENTZ, K. A., Pow, J. W., WRING, S. A., HUMPHREYS, J. E. and Pow, J. E., 2000, Influence of passive permeability on apparent P-glycoprotein kinetics. Pharmaceutical Research, 17, 1456–1460.
  • LOWRY, O. H., ROSEBRUGH, N. J., FARR, A. L. and RANDALL, R. J., 1951, Protein measurement with the folin phenol reagent. Journal of Biological Chemistry, 193, 265–275.
  • MANKHETKORN, S., DUBRU, F., HESSCHENBROUCK, J., FIALLO, M. and GARNIER-SUILLEROT, A., 1996, Relation among the resistance factor, kinetics of uptake, and kinetics of the P-glycoprotein-mediated efflux of doxorubicin, daunorubicin, 8-(S)-fluoroidarubicin, and idarubicin in multidrug-resistant K562 cells. Molecular Pharmacology, 49, 532–539.
  • MANKHETKORN, S. and GARNIER-SUILLEROT, A., 1998, The ability of verapamil to restore intracellular accumulation of anthracyclines in multidrug resistant cells depends on the kinetics of their uptake. European Journal of Pharmacology, 343, 313–321.
  • PAN, B. F., DUTT, A. and NELSON, J. A., 1994, Enhanced transepithelial flux of cimetidine by Madin-Darby canine kidney cells overexpressing human P-glycoprotein. Journal of Pharmacology and Experimental Therapeutics, 270, 1–7.
  • POLLI, J. W., WRING, S. A., HUMPHREYS, J. E., HUANG, L., MORGAN, J. B., WEBSTER, L. O. and SERABHT-SINGH, C. S., 2001, Rational use of in vitro P-glycoprotein assays in drug discovery. Journal of Pharmacology and Experimental Therapeutics, 299, 620–628.
  • REGEV, R. and EYTAN, G. D., 1997, Flip-flop of doxorubicin across erythrocyte and lipid membranes. Biochemical Pharmacology, 54, 1151–1158.
  • SAITOH, H. and AUNGST, B. J., 1995, Possible involvement of multiple P-glycoprotein-mediated efflux systems in the transport of verapamil and other organic cations across rat intestine. Pharmaceutical Research, 12, 1304–1310.
  • SARKADI, B., MULLER, M., HOMOLYA, L., HOLLO, Z., SEPRODI, J., GERMANN, U. A., GOTTESMAN, M. M., PRICE, E. M. and BOUCHER, R. C., 1994, Interaction of bioactive hydrophobic peptides with the human multidrug transporter. FASEB Journal, 8,766–770.
  • SAUNA, Z. E. and AMBUDKAR, S. V., 2000, Evidence for a requirement for ATP hydrolysis at two distinct steps during a single turnover of the catalytic cycle of human P-glycoprotein. Proceedings of the National Academy of Sciences, USA, 97, 2515–2520.
  • SAUNA, Z. E. and AMBUDKAR, S. V., 2001, Characterization of the catalytic cycle of ATP hydrolysis by human P-glycoprotein: the two ATP hydrolysis events in a single catalytic cycle are kinetically similar but affect different functional outcomes. Journal of Biological Chemistry, 276, 11653–11661.
  • SCALA, S., AKHMED, N., RAO, U. S., PAULL, K., LAN, L. B., DICKSTEIN, B., LEE, J. S., ELGEMEIE, G. H., STEIN, W. D. and BATES, S. E., 1997, P-glycoprotein substrates and antagonists cluster into two distinct groups. Molecular Pharmacology, 51,1024–1033.
  • SCHINKEL, A. H., WAGENAAR, E., MOL, C. A. and VAN DEEMTER, L., 1996, P-glycoprotein in the blood-brain barrier of mice influences the brain penetration and pharmacological activity of many drugs. Journal of Clinical Investigation, 97, 2517–2524.
  • SCHUETZ, E. G., YASUDA, K., ARIMORI, K. and SCHUETZ, J. D., 1998, Human MDR1 and mouse mdrla P-glycoprotein alter the cellular retention and disposition of erythromycin, but not of retinoic acid or benzo(a)pyrene. Archives of Biochemistry and Biophysics, 350, 340–347.
  • SHAPIRO, A. B. and LING, V., 1998, Stoichiometry of coupling of rhodamine 123 transport to ATP hydrolysis by P-glycoprotein. European Journal of Biochemistry 254, 189–193.
  • SMIT, J. W., WEERT, B., SCHINKEL, A. H. and MEIJER, D. K., 1998, Heterologous expression of various P-glycoproteins in polarized epithelial cells induces directional transport of small (type 1) and bulky (type 2) cationic drugs. Journal of Pharmacology and Experimental Therapeutics, 286, 321–327.
  • SOARES-DA-SILVA, P. and SERRAO, M. P., 2000, Outward transfer of dopamine precursor L-3,4-dihydroxyphenylalanine (L-dopa) by native and human P-glycoprotein in LLC-PK(1) and LLC-GA5 co1300 renal cells. Journal of Pharmacology and Experimental Therapeutics, 293,697–704.
  • SONVEAUX, N., VIGANO, C., SHAPIRO, A. B., LING, V. and RUYSSCHAERT, J. M., 1999, Ligand-mediated tertiary structure changes of reconstituted P-glycoprotein. A tryptophan fluorescence quenching analysis. Journal of Biological Chemistry, 274, 17649–17654.
  • STEIN, W. D., 1997, Kinetics of the multidrug transporter (P-glycoprotein) and its reversal. Physiology Reviews, 77, 545–590.
  • TANAKA, K., HIRAI, M., TANIGAWARA, Y., YASUHARA, M., HORI, R., UEDA, K. and INui, K., 1996, Effect of cyclosporin analogues and FK506 on transcellular transport of daunorubicin and vinblastine via P-glycoprotein. Pharmaceutical Research, 13, 1073–1077.
  • URBATSCH, I. L., AL-SHAWI, M. K. and SENIOR, A. E., 1994, Characterization of the ATPase activity of purified Chinese hamster P-glycoprotein. Biochemistry, 33, 7069–7076.
  • WANDEL, C., KIM, R., WOOD, M. and WOOD, A., 2002, Interaction of morphine, fentanyl, sufentanil, alfentanil, and loperamide with the efflux drug transporter P-glycoprotein. Anesthesiology, 96, 913–920.
  • WANG, E.-J., CASCIANO, C. N., CLEMENT, R. P. and JOHNSON, W. W., 2000a, Two transport binding sites of P-glycoprotein are unequal yet contingent: initial rate kinetic analysis by ATP hydrolysis demonstrates intersite dependency. Biochimica et Biophysica Acta, 1481, 63–74.
  • WANG, E.-J., CASCIANO, C. N., CLEMENT, R. P. and JOHNSON, W. W., 2000b, Cooperativity in the inhibition of P-glycoprotein-mediated daunorubicin transport: evidence for half-of-the-sites reactivity. Archives of Biochemistry and Biophysics, 383,91–98.
  • WANG, E.-J., CASCIANO, C. N., CLEMENT, R. P. and JOHNSON, W. W., 2000c, In vitro flow cytometry method to quantitatively assess inhibitors of P-glycoprotein. Drug Metabolism and Disposition, 28, 522–528.
  • WANG, E.-J., CASCIANO, C. N., CLEMENT, R. P. and JOHNSON, W. W., 2001a, HMG-CoA reductase inhibitors (statins) characterized as direct inhibitors of P-glycoprotein. Pharmaceutical Research, 18, 800–806.
  • WANG, E.-J., LEW, K., BARECKI, M., CASCIANO, C. N., CLEMENT, R. P. and JOHNSON, W. W., 2001b, Quantitative distinctions of active site molecular recognition by P-glycoprotein and cytochrome P450 3A4. Chemical Research and Toxicology, 14, 1596–1603.
  • WANG, E.-J., LEW, K., CASCIANO, C. N., CLEMENT, R. P. and JOHNSON, W. W., 2002, Characterization of common. azole antifungals contrasted for interaction with P-glycoprotein. Antimicrobial Agents and Chemotherapy, 46, 160–165.
  • WIELINGA, P. R., WESTERHOFF, H. V. and LANKELMA, J., 2000, The relative importance of passive and P-glycoprotein mediated anthracycline efflux from multidrug-resistant cells. European Journal of Biochemistry, 267, 649–657.
  • WOLF, D. C. and HORWITZ, S. B., 1992, P-glycoprotein transports corticosterone and is photoaffinity-labeled by the steroid. International Journal of Cancer, 52, 141–146.
  • YANG, J. J., Kim, K. J. and LEE, V. H., 2000, Role of P-glycoprotein in restricting propranolol transport in cultured rabbit conjunctival epithelial cell layers. Pharmaceutical Research, 17, 533–538.
  • YUSA, K. and TSURUO, T., 1989, Reversal mechanism of multidrug resistance by verapamil: direct binding of verapamil to P-glycoprotein on specific sites and transport of verapamil outward across the plasma membrane of K562/ADM cells. Cancer Research, 49, 5002–5006.
  • ZACHOWSKI, A., 1993, Phospholipids in animal eukaryotic membranes: transverse asymmetry and movement. Biochemical Journal, 294, 1–14.
  • ZSCHIESCHE, M., LEMMA, G. L., KLEBINGAT, K. J., FRANKE, G., TERHAAG, B., HOMANN, A., GRAMATTE, T., KROEMER, H. K. and SIEGMUND, W., 2002, Stereoselective disposition of talinolol in man. Journal of Pharmaceutical Science, 91, 303–311.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.